Artificial tears and therapeutic uses

a technology of artificial tears and therapeutic uses, applied in the field of artificial tears, can solve the problems of eye surface, increased discomfort and sensitivity to bright light, and affects both eyes

Active Publication Date: 2013-07-30
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The damage to the eye surface resulting from dry eye increases discomfort and sensitivity to bright light and both eyes usually are affected.
Because blinking coats the eye with tears, symptoms are worsened by activities in which the rate of blinking is reduced due to prolonged use of the eyes.
However, if the condition is left untreated or becomes severe, it can produce complications that can cause eye damage, resulting in impaired vision or possibly in the loss of vision.
Having dry eyes for a prolonged period of time can lead to tiny abrasions on the surface of the eyes.
Some severe cases result in thickening of the corneal surface, corneal erosion, punctate keratopathy, epithelial defects, corneal ulceration, corneal neovascularization, corneal scarring, corneal thinning, and even corneal perforation.
An abnormality of any one of the three layers of tears which produces an unstable tear film, may result in symptoms of keratitis sicca.
Keratoconjunctivitis sicca is usually due to inadequate tear production.
The aqueous tear layer is affected, resulting in aqueous tear deficiency or lacrimal hyposecretion.
The lacrimal gland does not produce sufficient tears to keep the entire conjunctiva and cornea covered by a complete layer.
Keratoconjunctivitis sicca can also be caused by abnormal tear composition resulting in rapid evaporation or premature destruction of the tears.
In this condition, although the tear gland produces a sufficient amount of tears, the rate of evaporation of the tears is too rapid.
There is a loss of water from the tears that results in tears that are too “salty” or hypertonic.
As a result, the entire conjunctiva and cornea cannot be kept covered with a complete layer of tears during certain activities or in certain environments.
This is due to the fact that tear production decreases with age.
Diabetics are also at increased risk for dry eye.
Disorders of the eyelid can impair the complex blinking motion required to spread tears.
Dry eyes caused by these procedures usually disappear after several months.
Lubricating tear ointments can be used during the day, but they generally are used at bedtime due to poor vision after application.

Method used

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  • Artificial tears and therapeutic uses

Examples

Experimental program
Comparison scheme
Effect test

example 1

Manufacturing Procedure for Emulsion Compositions of this Invention

[0033]As disclosed below, the emulsion compositions of this invention may be manufactured with and without tonicity components, such as glycerin, erythritol, carnitine, etc.

[0034]Batches were manufactured on a weight basis from pre-weighed compendial raw materials in five parts:

[0035]Part 1: an oil phase containing a mixture of castor oil and olive oil (non-sterile).

[0036]Part 2: an aqueous phase containing purified water, polysorbate 80, and glycerin. Part 2 is sterile filtered using a sterile Nalgene filtration unit with a 0.2 μm PES membrane.

[0037]Part 3: an aqueous polymer dispersion containing purified water and Pemulen® TR-2

(5× Stock solution, 0.5%). Part 3 is sterilized by autoclaving at 121° C. for 15 minutes at 15 psig.

[0038]Part 4: an aqueous polymer dispersion containing purified water and sodium carboxymethylcellulose. (5× Stock solution, 2.5%). Part 4 is sterilized by autoclaving at 121° C. for 15 minute...

example 2

Testing of Oil Mixtures for Ability to Spread on Ocular Surface Drop Dispersion Procedure

[0049]1. “Model Tear Solution”, described in Table 2, below, is added to of a small cell culture dish (25 mm×10 mm style) in an amount sufficient to cover the bottom thereof. Amount should be ˜2.5 mL);[0050]2. One drop of oil mixture (10 to 50 μl drop size) is added to said dish and an observation of how readily the drop disperses on the surface of the tear solution is made for not less then 60 seconds;[0051]3. The drop dispersed on the tear solution surface is mixed with a spatula and how readily the drop disperses in the tear solution is observed; and,[0052]4. The mixed oil and tear solution observe for several minutes / hours to see if oil coalesces.

[0053]

TABLE 2Composition of Model Tear SolutionIngredientConc. (% w / v)Sodium Chloride0.90Calcium Chloride, Dihydrate0.015Sodium Phosphate Dibasic, Heptahydrate0.028Lysozyme, egg white0.19Albumin, bovine0.020Gamma-Globulin, human0.010Mucin, bovine su...

example 3

Summary of 1-Day Ocular Tolerability Study of an Emulsion of Example 2 in Rabbits

[0058]A 1-day ocular tolerability study of an emulsion comprising 0.25%, by weight, of a 70 / 30 castor oil / olive oil mixture, manufactured according to Example 1, was conducted in rabbits. The oil mixture was utilized as a vehicle for the tonicity components carnitine, glycerine and erythritol. Female New Zealand White rabbits (5 rabbits / group) were given one drop (˜40 μL each drop) of said emulsion of or a marketed, comparator eye drop, comprising 1.25%, by weight, castor oil, emulsified in an aqueous phase, by topical ocular instillation in the left eye (OS), 6 times daily (approximately 1 hr intervals) for one day. The contralateral right eye (OD) served as a control without eye drop instillation. The following parameters were evaluated: viability, clinical observations, ocular discomfort, gross ocular observations (irritation), and ophthalmic examination (slit lamp biomicroscopy, pupillary reflex). O...

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Abstract

The present invention provides ophthalmic compositions, e.g. artificial tears, suitable for treating dry eye syndrome in a human or other mammal suffering there from, e.g. a dog or cat, which comprise a mixture of castor oil with another oil, e.g. a food oil, e.g. olive oil, sesame oil, corn oil etc.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This is a national stage application under 35 U.S.C. §371 of PCT patent application PCT / US10 / 37153, filed on Jun. 3, 2010, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61 / 184,339, filed on Jun. 5, 2009, each of which is hereby incorporated by reference in its entirety.BACKGROUND OF THE INVENTION[0002]1. Field of the Invention[0003]The present invention is directed to artificial tears suitable for treating dry eye syndrome in a human or other mammal which comprises a mixture of castor oil with at least one other oil, for example a naturally occurring oil (e.g. olive oil, sesame oil, corn oil, etc.)[0004]2. Description of Related Art[0005]Typical symptoms of keratoconjunctivitis or dry eye include feelings of dryness, burning, and a sandy-gritty eye sensation that can worsen during the day. Symptoms may also be described as itchy, scratchy, stingy or tired eyes. Other symptoms include pain, redness, a pulling sen...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A01N65/00
CPCA61K36/47A61K9/0048A61K36/55A61K47/44A61K9/107A61P27/00A61P27/02A61P27/04
Inventor GORE, ANURADHA V.JORDAN, ROBERT S.KROCK, KEVINPUJARA, CHETAN P.
Owner ALLERGAN INC
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